Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.

@article{Ct2007SubstitutedPI,
  title={Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.},
  author={Bernard C{\^o}t{\'e} and Louise Boulet and Christine Brideau and David Claveau and Diane Ethier and R. Frenette and Marc Gagnon and Andr{\'e} Giroux and Jocelyne Guay and S{\'e}bastien Guiral and J C M A Mancini and Evelyn Martins and Fr{\'e}d{\'e}ric Mass{\'e} and Nathalie M{\'e}thot and Denis Riendeau and Joel E. Rubin and Daigen Xu and Hongping Yu and Yves Ducharme and Richard W. Friesen},
  journal={Bioorganic & medicinal chemistry letters},
  year={2007},
  volume={17 24},
  pages={6816-20}
}
Phenanthrene imidazole 3 (MF63) has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor. This new series was developed by lead optimization of a hit from an internal HTS campaign. Compound 3 is significantly more potent than the previously reported indole carboxylic acid 1 with an A549 whole cell IC(50) of 0.42 microM (50% FBS) and a human whole blood IC(50) of 1.3 microM. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model when orally… CONTINUE READING

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